CN1655771A - At least partially degradable films containing an active ingredient and method for the production thereof - Google Patents

At least partially degradable films containing an active ingredient and method for the production thereof Download PDF

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Publication number
CN1655771A
CN1655771A CNA038117258A CN03811725A CN1655771A CN 1655771 A CN1655771 A CN 1655771A CN A038117258 A CNA038117258 A CN A038117258A CN 03811725 A CN03811725 A CN 03811725A CN 1655771 A CN1655771 A CN 1655771A
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CN
China
Prior art keywords
film
reactive compound
described film
layer
active ingredient
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CNA038117258A
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Chinese (zh)
Inventor
G·赫林
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Agfa Gevaert AG
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Agfa Gevaert AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Agfa Gevaert AG filed Critical Agfa Gevaert AG
Publication of CN1655771A publication Critical patent/CN1655771A/en
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7007—Drug-containing films, membranes or sheets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A novel administration form of active ingredients, especially active ingredients having a pharmacological or biocidal effect, in the form of a film containing at least one active ingredient which is at least partially degraded by the conditions in the place of action.

Description

Contain reactive compound and to degradable film of small part and preparation method thereof
The present invention relates to a kind of compositions, wherein contain at least a reactive compound, described at least a reactive compound can discharge in accurate adjustable mode.
Reactive compound among the present invention is a low molecular weight organic compound, after it disengages from compositions, has given play to the effect of expectation, particularly pharmacology or Biocide effect.
Pharmaceutical active compounds (medicine) can multiplely can make this pharmaceutical active compounds expect that in expeced time the dosage form of organism site performance projected dose effect exists.And above-mentioned purpose is that often institute is irrealizable for the known formulations form.
Therefore, a permanent purpose is exactly the new improvement dosage form that development can realize specific purposes and dosage.
The present invention realizes above-mentioned purpose by a kind of film, contains at least a reactive compound in the described film, and this film is degraded down to small part in the condition of institute's action site.
Preferably, described film is made by biomaterial, for example by the polypeptide of randomly part degraded, particularly made by gelatin.Described biomaterial preferably can be at the action site enzymatic degradation, thereby by this mode at least a release active compound of being stored in the film is come out.
The biomaterial of described film can carry out modification by following means, for example by aqueous polymer emulsion or polymeric dispersions, by water solublity and optional crosslinkable polymer or copolymer or protein derivatives.The 598th page of Res.Discl.38957 (1996) seen in the description of the example of these method of modifying, II A Zhanghe II C chapter, comprising, for example, polyacrylamide, polyacrylic acid derivative, polyvinylpyrrolidone, polyvinyl alcohol, polyvinyl imidazole, poly(ethylene oxide), polystyrolsulfon acid or cellulose derivative.In addition; can also further described biomaterial be solidified to some extent promptly crosslinked; for example; crosslinked with divinylsulfone, aldehyde, cyanuric chloride or epoxide by amino; perhaps crosslinked with carbodiimide or carbamoyl pyridium salt, perhaps crosslinked by carboxyl with aziridine derivative by carboxyl and amino.957 (1996) the 599th pages of Res.Discl.38, II chapter, B are seen in the description of other proper curing agents.
The film that biomaterial is made, the particularly film made from gelatin have multiple advantage: they can be made
Thin layer,
Accurate layer,
Multilamellar,
Layer with predetermined properties,
Flexible layer.
Particularly following being prepared promptly will be made the biomaterial that film uses with suitable casting equipment and be cast on the carrier film with the aqueous solution form, after the drying it be uncovered.Preferably, use stepwise or curtain formula pouring attachment to carry out continuously.
Casting equipment is for example known by the preparation of photographic material.
Preferred carrier film has, and tri cellulose acetate membrane and tow sides have all applied poly paper, these the two kinds known carrier materials that all can be used as photographic material.In addition, polyester (PET or PEN) or polycarbonate membrane also can use.
Different with photographic material, because that layer that cast will be got on after making is uncovered, so be unworthy of putting substrate layer or adhesion layer in described carrier film, the purpose of substrate layer or adhesion layer is that the layer that will pour into a mould subsequently is attached on the carrier film.
Described reactive compound is added cast solution, introduce in subsequently the film in this mode then.Can guarantee that like this dosage is accurate.In addition, described reactive compound for example can be distributed under specific environment in the solution introduce high boiling organic solvent for example, this solvent can emulsifying in moisture cast solution.
Also reactive compound can be imported with material filling latex form in addition.In this case, flood or fill latex with water soluble active compound.The 623rd page of Res.Discl.38957 (1996) seen in be used to the to photograph description of colour coupler of this introduction method.
Film of the present invention can constitute by several layers.If when comprising at least two kinds of mutual exclusive reactive compounds in film, the advantage of this structure has just displayed, because chemical compound can be imported different layers.In addition, reactive compound can also be provided at different layers with variable concentrations, thereby make that reactive compound can discharge by different amount regulation and control in the process of using subsequently.
In order to prepare the pharmaceutical formulation form, described film can be cut into and use for a short time with part minimum and in this mode, being contained in these parts can be that solid also can be liquid preparation form, for example tablet or medicine juice.
In addition, can also be with the form of large stretch of film as plaster.
Release is undertaken by the membrane substance degraded, with regard to gelatin film, is to be undertaken by enzymatic degradation, particularly the biological intravital enzyme for the treatment of by reactive compound, for example trypsin.
If reactive compound will be used especially slowly; to realize the special degraded at a slow speed of film with it adaptably; the protective layer that can not degrade can be provided at the tow sides of this film; this protective layer also can result from the preparation process, and the release of degraded and reactive compound can only be undertaken by the cut edge of small pieces film.
From the above mentioned, also have other single or several reactive compounds may be raised the supply organism in the expectation mode certainly.
Embodiment
The preparation of reactive compound Emulsion
Emulsion 1
9g Metipranolol and 10.0g olive oil are dissolved in the 70.0g ethyl acetate, and under 40 ℃, in 10 minutes time, this emulsifying soln is gone into the aqueous solution of forming by following material: 10.0g gelatin, 350g water and 0.5g dodecyl benzene sulfonate by emulsifying device.Ethyl acetate is evaporated in this course, obtains O/W Emulsion, adds water to 500g.
Emulsion 2
9g Betaxolol and 90.0g olive oil are dissolved in the 80g ethyl acetate, and under 40 ℃, in 12 minutes time, this emulsifying soln is gone into the aqueous solution of forming by following material: 6.0g gelatin, 350g water and 0.5g dodecyl benzene sulfonate by emulsifying device.Ethyl acetate is evaporated in this course, obtains O/W Emulsion, adds water to 500g.
The preparation of reactive compound potting syrup
Potting syrup 1
Under 40 ℃, 66g 20 weight % gelatin, 90g water and 4.0g 10 weight % dioctylsulfosuccinat, Na saline solution (wetting agent) are added 160g Emulsion 1, water is mended mixture full of 350g.
Potting syrup 2
Under 40 ℃, 70g 20 weight % gelatin, 90g water and 4.0g 10 weight % dioctylsulfosuccinat, Na saline solution (wetting agent) are added 160g Emulsion 2, water is mended mixture full of 350g.
Curing agent solution
9.2g bi-vinyl sulfonyl methane is dissolved in the mixture of the 450g that is made up of 30g ethanol and 420g water, adds the 10 weight % wetting agent solution of 6g then based on triterpenoid (saponin).
But the film of enzymatic degradation
Use the known stepwise pouring attachment that can be used for preparing photographic material, on the polyethylene terephthalate film of no substrate, be coated with:
1. potting syrup 1
2. potting syrup 2
3. potting syrup 1
4. curing agent solution
The standard of the coating weight that the present invention selects for use is that the coating weight in 3 layers of complex that obtain after 50 ℃ of dryings is respectively:
Layer 1 10g/m 2
Layer 2 20g/m 2
Layer 3 10g/m 2
Uncover non--adhering composite bed from polyethylene terephthalate film, and be cut to the big or small 1mm that is 2Sheet.
Reactive compound selectivity release test
1. the above-mentioned diaphragm of 0.5g is scattered in the buffered water of 100g pH8, dispersion liquid was stirred 1 hour down at 20 ℃.Filter then, analyze filtrate.Do not find reactive compound.
2. the above-mentioned diaphragm of 0.5g is scattered in the buffered water of 100g pH8, adds 10g 3 weight % trypsin solutions, dispersion liquid is stirred down at 20 ℃.In (sample 1) after 10 minutes and (sample 2) sampling after 60 minutes, filter, analyze filtrate.
The result:
Only contain Metipranolol in the sample 1
Contain Metipranolol and Betaxolol in the sample 1.
This test shows: diaphragm is by enzymatic degradation effect release of active compounds in succession optionally.

Claims (12)

1. film that contains a kind of reactive compound at least, this film is degraded down to small part in the action site condition.
2. the described film of claim 1 is characterized in that described reactive compound is a kind of low-molecular-weight organic compound.
3. claim 1 or 2 described films is characterized in that described reactive compound has a kind of effect at organism.
4. the described film of claim 3 is characterized in that wherein said effect is a kind of pharmacological action.
5. the described film of claim 1 is characterized in that this film made by biomaterial.
6. the described film of claim 5 is characterized in that this film is to be made by the polypeptide of part degraded.
7. the described film of claim 6, but it is characterized in that this film is an enzymatic degradation.
8. the described film of claim 1 is characterized in that it has only one deck.
9. the described film of claim 1 is characterized in that this film is made up of multilamellar.
10. the described film of claim 9 is characterized in that importing in described each layer at least a reactive compound of variable concentrations.
11. the described film of claim 9 is characterized in that importing in described each layer multiple different reactive compound.
12. be used for preparing the method for each described film of claim 1-11, it is characterized in that the aqueous solution that will contain the material that the system film of at least a active substance uses with suitable casting equipment is cast on the carrier film, drying is taken off it then and is got from carrier film.
CNA038117258A 2002-05-24 2003-04-04 At least partially degradable films containing an active ingredient and method for the production thereof Pending CN1655771A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10223435.3 2002-05-24
DE10223435 2002-05-24

Publications (1)

Publication Number Publication Date
CN1655771A true CN1655771A (en) 2005-08-17

Family

ID=29557316

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA038117258A Pending CN1655771A (en) 2002-05-24 2003-04-04 At least partially degradable films containing an active ingredient and method for the production thereof

Country Status (6)

Country Link
US (1) US20060134184A1 (en)
EP (1) EP1519718A1 (en)
JP (1) JP2005531569A (en)
CN (1) CN1655771A (en)
AU (1) AU2003240762A1 (en)
WO (1) WO2003099263A1 (en)

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2966275D1 (en) * 1978-11-07 1983-11-10 Beecham Group Plc Device for oral administration to a ruminant animal
JPS5647761A (en) * 1979-09-27 1981-04-30 Fuji Photo Film Co Ltd Laminated analyzing piece and immunity analyzing method using the same
DE69004415D1 (en) * 1990-03-05 1993-12-09 Minnesota Mining & Mfg Device for delayed delivery of pharmacologically active compounds into the ear.
GB2280850B (en) * 1993-07-28 1997-07-30 Johnson & Johnson Medical Absorbable composite materials for use in the treatment of periodontal disease
US5800832A (en) * 1996-10-18 1998-09-01 Virotex Corporation Bioerodable film for delivery of pharmaceutical compounds to mucosal surfaces
DE19646392A1 (en) * 1996-11-11 1998-05-14 Lohmann Therapie Syst Lts Preparation for use in the oral cavity with a layer containing pressure-sensitive adhesive, pharmaceuticals or cosmetics for dosed delivery
DE19960154A1 (en) * 1999-12-14 2001-07-12 Lohmann Therapie Syst Lts Flat pharmaceutical preparation for transmucosal administration of oxycodone or a comparable active ingredient in the oral cavity, for use in pain therapy and addiction therapy
WO2003020191A1 (en) * 2001-09-04 2003-03-13 University Of Iowa Research Foundation Cellulose membranes for biodegradable scaffolds
US7204994B2 (en) * 2003-02-03 2007-04-17 Ashland Licensing And Intellectual Property Llc Juvenile hormone compositions and methods for making same

Also Published As

Publication number Publication date
JP2005531569A (en) 2005-10-20
WO2003099263A1 (en) 2003-12-04
US20060134184A1 (en) 2006-06-22
EP1519718A1 (en) 2005-04-06
AU2003240762A1 (en) 2003-12-12

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